Bupropion: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on Nov 20, 2023.

1. How it works

• Bupropion is an antidepressant that may also be used to help people quit smoking.
• Experts do not know exactly how bupropion works in depression but historically it was thought to be due to its ability to inhibit the reuptake of two neurotransmitters, norepinephrine, and dopamine (although this reuptake inhibition is weak). Bupropion does not affect the reuptake of serotonin or inhibit monoamine oxidase. Studies confirm that bupropion is still effective for treating mood disorders, such as depression, even though the way it works is unknown.
• Bupropion is thought to be effective for smoking cessation because of its ability to increase dopamine levels in the nerve synapse by inhibiting the reuptake of dopamine. This replaces the dopamine deficiency experienced during nicotine withdrawal (nicotine causes a release of dopamine which enhances the pleasure-seeking pathways in the brain; reducing nicotine intake means these pathways are no longer being stimulated; bupropion counteracts this effect).
• Bupropion is an aminoketone antidepressant and is chemically unrelated to any other type of antidepressant.

2. Upsides

• Bupropion (Wellbutrin [discontinued], Aplenzin, and generic bupropion) may be used to relieve the symptoms of depression in Major Depressive Disorder (MDD) and Seasonal Affective Disorder (SAD).
• May be considered second-line for the treatment of bipolar depression when first-line agents are not effective or tolerated.
• Bupropion (Zyban brand [discontinued], generic bupropion) may be used to relieve cravings associated with nicotine withdrawal during smoking cessation. Research has shown that treatment with bupropion is significantly more effective at helping people to quit smoking than no treatment. Bupropion may also be combined with a Nicotine Transdermal System (nicotine patches), although blood pressure should be monitored.
• May be used off-label (not an FDA-approved use but considered by some expert organizations as an option if standard treatments are not effective or tolerated) for attention deficit hyperactivity disorder (ADHD).
• Generic bupropion is available (for depression or smoking cessation) and bupropion is also marketed under the brand name Aplenzin (for depression).

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Insomnia, headache, dizziness, dry mouth, sore throat, nausea, and constipation are the more commonly reported side effects. May also cause abdominal pain, abnormal dreams, flushing, muscle and joint pain, migraine, rash, or itchy skin.
• Severe neuropsychiatric symptoms, including agitation, anxiety, delusions, hallucinations, panic disorder, paranoia, and psychosis have been reported with bupropion use and it carries a black box warning for these effects. Symptoms have occurred in people with and without pre-existing psychiatric disease. People should be monitored for the appearance of neuropsychiatric symptoms. Most cases resolved on discontinuation of bupropion; however, a few persisted.
• More likely than other antidepressants to cause weight loss; however, may also cause weight gain in some people.
• May increase blood pressure. Blood pressure should be taken on treatment initiation and monitored periodically.
• The dosage of bupropion requires adjusting for kidney and liver disease. Active metabolites may accumulate and increase the risk of seizures.
• Conventional tablets may need to be taken up to three times daily. Preferably at least 6 hours should separate doses (eg, in the morning, midday, and in the evening). Avoid bedtime administration of the evening dose to reduce the incidence of insomnia. Dosages of 300mg or more should be split into divided doses that do not exceed 150mg each.
• Extended-release tablets should be administered twice daily (but may be administered once daily on initiation).
• May not be suitable for some people including those with seizure disorders; eating disorders; undergoing alcohol, anticonvulsant, barbiturate, or benzodiazepine withdrawal; at risk of glaucoma; already taking bupropion for another indication (such as smoking cessation); pregnant or breastfeeding; or a history of allergy to bupropion or monoamine oxidase inhibitor use within the past two weeks.
• Not approved for use in children under the age of 18 years.
• As with other antidepressants, bupropion may increase the risk of suicidal thoughts or behavior. The risk is greatest for children and young adults under the age of 24. Monitor for worsening mood.
• May increase the risk of seizures. This risk is increased with higher dosages of bupropion, in those with head injuries or taking other medications which also lower the seizure threshold.
• Not suitable for the treatment of panic disorder and concomitant phobic disorder but may improve symptoms of panic in those with depression. Not recommended for the treatment of bulimia nervosa because it has been associated with seizures in purging bulimic patients.
• May cause allergic reactions in some people with symptoms such as itchiness, facial swelling, and hives (urticaria). Stop treatment immediately and seek medical help.
• May cause a discontinuation syndrome if abruptly stopped or interrupted (symptoms include nausea, vomiting, diarrhea, headaches, dizziness, sweating, chills, tremors, vivid dreams, and insomnia).
• May interact with other drugs, such as other antidepressants and antipsychotics; agents that affect the electrical conductivity in the heart; those that induce or inhibit hepatic enzymes CYP2B6 or are metabolized by CYP2D6; other drugs that increase dopamine; or those that increase bleeding risk.
• Interaction with other medicines that increase serotonin levels (such as tramadol, other antidepressants, St John's wort) or overdosage may cause serotonin syndrome (symptoms include mental status changes [such as agitation, hallucinations, coma, delirium], fast heart rate, dizziness, flushing, muscle tremor or rigidity, and stomach symptoms [such as nausea, vomiting, diarrhea]).
• Rare cases of priapism (painful erections more than 6 hours in duration) have been reported.
• May cause false-positive results on urine screening tests for amphetamines.
• Not recommended during pregnancy. If a woman inadvertently becomes pregnant while taking bupropion, enroll her on the pregnancy registry at 800-336-2176. Breastfeeding is not recommended while taking bupropion.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Bupropion may be used in the treatment of depression or as an aid to smoking cessation; however, side effects may include insomnia, neuropsychiatric adverse events, or seizures. It carries a black box warning because it may cause changes in behavior and increase the risk of suicidal thoughts.

5. Tips

• Can be taken with or without food.
• Avoid taking the last dose of the day after 5pm to minimize the risk of insomnia. At least eight hours should separate twice daily dosings of bupropion, and at least six hours should separate three times daily dosings of bupropion. Take bupropion exactly as directed by your doctor.
• Regardless of whether bupropion is being used as an antidepressant or as a smoking cessation aid, it should be started at a low dose and tapered up slowly over several days. Your doctor will advise you how to do this. Controlled-release forms of bupropion should be swallowed whole. Do not crush, divide, or chew because this may increase the risk of adverse effects including seizures.
• Generic bupropion contains the same active ingredient as Aplenzin, which is also bupropion, and the two should never be used together.
• Bupropion may affect your judgment and your ability to drive or operate machinery. Avoid performing hazardous tasks such as driving if bupropion has this effect on you.
• If you are using bupropion as an aid to stopping smoking, start treatment while you are still smoking, and at least one week (maximum of two weeks) before your planned quit day, to ensure that the concentration of bupropion in your body is at an effective level. You should aim for complete abstinence (no smoking at all past your quit day).
• If you have been taking bupropion for 7 to 12 weeks and have still not quit smoking, it is unlikely you will do so, and you should talk to your doctor about discontinuing it and reassessing other treatment options. However, some people may benefit from more than 12 weeks of bupropion treatment. In addition to bupropion treatment for smoking cessation, counseling, and other support to help you quit the habit is important. Do not be discouraged if your first attempt at quitting smoking fails. Studies have estimated it may take up to 30 attempts for some smokers to successfully quit. Try again when conditions are more favorable.
• When used to treat Seasonal Affective Disorder (SAD), bupropion should be initiated in the autumn before the onset of depressive symptoms, continued throughout the winter season, and tapered off in early spring.
• Be alert for changes in behavior or mood including agitation, depression, or suicide-related events. Seek immediate medical advice if any changes are apparent.
• Stop taking bupropion if any symptoms suggestive of an allergic reaction occur (such as itchiness, body rash, swelling) and seek immediate medical help.
• See your doctor immediately if you develop any eye pain, visual disturbances, swelling, or redness around the eye.
• If using bupropion for depression, do not stop abruptly unless on a doctor's advice or if an allergic reaction occurs. If you need to discontinue bupropion, your doctor will advise you how to do so slowly.
• Minimize or avoid consumption of alcohol as your tolerance to it may be diminished while taking bupropion, and it may also increase the risk of neuropsychiatric adverse events.
• Talk to your doctor or pharmacist before you take any other medication with bupropion, including those bought over the counter.
• Bupropion is not recommended during pregnancy or breastfeeding. Contact your doctor immediately if you inadvertently become pregnant while taking bupropion.

6. Response and effectiveness

• When bupropion is used for depression, improvements in sleep, energy, or appetite may be apparent within the first 1-2 weeks. Depressed mood or motivation may take up to 6-8 weeks to fully improve.
• Bupropion decreases nicotine cravings and withdrawal symptoms but effects take about one to two weeks to develop.
• Bupropion is metabolized to three active metabolites once in the body, each with varying durations of action.

7. Interactions

Medicines that interact with bupropion may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with bupropion. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with bupropion include:

• amantadine
• antiarrhythmics, such as amiodarone or flecainide
• anticonvulsants, such as carbamazepine, phenytoin, phenobarbital, or primidone
• antidepressants, such as SSRIs (eg, fluoxetine, sertraline), tricyclic antidepressants (such as desipramine, nortriptyline), or MAOIs (such as phenelzine or selegiline) (these may lower the seizure threshold)
• antipsychotics (such as butyrophenones, phenothiazines, or thioxanthenes) and atypical antipsychotics (eg, olanzapine, quetiapine, ziprasidone)
• any medication that lowers the seizure threshold, such as corticosteroids, tramadol, reserpine, and volatile anesthetics
• benzodiazepines, such as diazepam, lorazepam, or oxazepam
• beta-blockers, such as atenolol or metoprolol
• blood thinners, such as clopidogrel or ticlopidine
• cimetidine
• corticosteroids, such as prednisone or methylprednisone
• cyclophosphamide
• HIV medications, such as efavirenz, ritonavir, or lopinavir
• levodopa
• nicotine
• orphenadrine
• theophylline
• warfarin.

Avoid drinking alcohol or taking illegal or recreational drugs while taking bupropion because it may increase the risk of neuropsychiatric side effects.

Medications that induce CYP2D6 such as dexamethasone or rifampin may reduce concentrations of bupropion and drugs that inhibit CYP2D6, such as amiodarone, celecoxib, or fluoxetine may increase concentrations of bupropion.

Note that this list is not all-inclusive and includes only common medications that may interact with bupropion. You should refer to the prescribing information for bupropion for a complete list of interactions.

References

• Bupropion. Revised 09/2023. Solco Healthcare US, LLC. https://www.drugs.com/pro/bupropion.html
• Aplenzin (bupropion) (Package Insert). Revised 06/2022. Bausch Health Companies Inc. https://www.drugs.com/pro/aplenzin.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use bupropion only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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